title: Synthesis of benzologues of Nitazoxanide and Tizoxanide: a comparative study of their in vitro broad-spectrum antiprotozoal activity.
abstract: We have synthesized two new benzologues of Nitazoxanide (NIT) and Tizoxanide (TIZ), using a short synthetic route. Both compounds were tested in vitro against six protozoa (Giardia intestinalis, Trichomonas vaginalis, Entamoeba histolytica, Plasmodium berghei, Leishmania mexicana and Trypanosoma cruzi). Compound 1 (benzologue of NIT) showed broad antiprotozoal effect against all parasites tested, showing IC(50)'s<5 μM. This compound was five-times more active than NIT, and 18-times more potent than metronidazole against G. intestinalis. It was 10-times more active than pentamidine against L. mexicana, and it was sevenfold more potent than benznidazole versus T. cruzi. This compound could be considered as a new broad spectrum antiprotozoal agent.
authors.affiliation: Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos 62209, Mexico. gabriel_navarrete@uaem.mx
authors.forename: Gabriel
authors.initials: G
authors.lastname: Navarrete-Vazquez
authors.forename: Fabiola
authors.initials: F
authors.lastname: Chávez-Silva
authors.forename: Rocío
authors.initials: R
authors.lastname: Argotte-Ramos
authors.forename: María del Carmen
authors.initials: Mdel C
authors.lastname: Rodríguez-Gutiérrez
authors.forename: Manuel Jesús
authors.initials: MJ
authors.lastname: Chan-Bacab
authors.forename: Roberto
authors.initials: R
authors.lastname: Cedillo-Rivera
authors.forename: Rosa
authors.initials: R
authors.lastname: Moo-Puc
authors.forename: Emanuel
authors.initials: E
authors.lastname: Hernández-Nuñez
mesh_terms: D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D005872:Giardia / Q000187:drug effects; D015394:Molecular Structure; D009574:Nitro Compounds; D010961:Plasmodium / Q000187:drug effects; D013844:Thiazoles / Q000138:chemical synthesis / Q000494:pharmacology; D014246:Trichomonas vaginalis / Q000187:drug effects
chemical_list: D000981:Antiprotozoal Agents; D009574:Nitro Compounds; D013844:Thiazoles; C104067:tizoxanide; C041747:nitazoxanide